JARID1 (Jumonji AT-Rich Interactive Domain 1) inhibitor (IC50
values are 3, 4.9 and 6 μ
M for JARID1B, 1A and 1C, respectively). Selective for JARID1 over UTX and JMJD3. Increases levels of methylated H3K4 in JARIDB1-transfected HeLa cells and MCF7 cells. Inhibits proliferation of breast cancer cell lines expressing high levels of JARIDB1.
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Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen.
Sayegh et al.